To prepare temperature and pH dual-responsive drug delivery systems, the thermosensitive polymer poly(N-isopropylacrylamide) (PNIPAAm) was first synthesized by free-radical polymerization. It was then co-dissolved with the pH-sensitive polymer Eudragit® L 100-55 (EL100-55) and processed into fibers using electrospinning. Ketoprofen (KET), a model drug, was also incorporated into the composite fibers, and fibers based on a single polymer additionally prepared. The fibers had smooth cylindrical morphologies, and no obvious phase separation could be seen...

Assessment of the impact of pharmaceutical residues on living organisms is a very complex subject. Apart from taking into account the toxicity of individual compounds, environmental factors should also be taken into account. In this paper, attempts were made to assess the impact of coexisting inorganic ions and changes in pH on the toxicity of ten selected pharmaceuticals. Two bioassays were used to measure the estrogenic and androgenic effects (XenoScreen YES/YAS - Saccharomyces cerevisiae) and acute toxicity (Microtox® - Vibrio fischeri)...

1) A novel method utilizing an internal standard in hepatocytes incubations has been developed and demonstrated to decrease the variability in the determination of intrinsic clearance in this system. The reduced variability was shown to allow differentiation of lower elimination rate constants from noise. 2) The suggested method was able to compensate for a small but systematic error (0.5 µL/min/106 cells) caused by an evaporation of approximately 15% of the volume during the incubation time. 3) The approach was validated using six commercial drugs (ketoprofen, tolbutamide, phenacetin, etodolac and quinidine) which were metabolized by different pathways...

INTRODUCTION: Adult renal colic is a frequent lombo-abdominal painful syndrome in emergencies. Treatment is based on nonsteroidal anti-inflammatory drug (NSAID) but the choice between different NSAIDs remains a subject of controversy. Our aim was to compare the efficacy and the safety of two intramuscularly NSAIDs in renal colic. METHODS: We conducted a 32-week, randomized, double-blind, single-center study . Patients who had renal colic with a visual analogue scale (VAS) ≥ 5 were randomly assigned to receive, by intramuscularly injection, 100 mg of Ketoprofen (GK) or 75 mg of diclofenac (GD)...

Emerging pollutants, including pharmaceutical compounds, are producing water pollution problems around the world. Some pharmaceutical pollutants, which mainly reach ecosystems within wastewater discharges, are persistent in the water cycle and can also reach the food chain. This work addresses this issue, accounting the grey component of the water footprint (GWFP ) for four of the most common pharmaceutical compounds (carbamazepine (CBZ), diclofenac (DCF), ketoprofen (KTP) and naproxen (NPX)). In addition, the GWFC for the main conventional pollutants is also accounted (nitrate, phosphates and organic matter)...

Inter-individual variability in warfarin dose requirement demands personalized medicine approaches to balance its therapeutic benefits (anticoagulation) and bleeding risk. Cytochrome P450 2C9 (CYP2C9) genotype-guided warfarin dosing is recommended in the clinic, given the more potent S-warfarin is primarily metabolized by CYP2C9. However, only about 20-30% of inter-patient variability in S-warfarin clearance is associated with CYP2C9 genotype. We evaluated the role of hepatic uptake in the clearance of R- and S-warfarin...

In this paper, parallel artificial liquid membrane extraction (PALME) was used for the first time to clean-up dried blood spots (DBS) prior to ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). Fundamental studies exploring amongst others desorption from the DBS in alkaline or acidic aqueous conditions, total extraction time and absolute recoveries were executed. Desorption and PALME were performed using a set of two 96-well plates, one of them housing the sample and the other comprising the supported liquid membrane (SLM) and the acceptor solution...

Non-steroidal anti-inflammatory drugs (NSAIDs) represent a growing concern for marine ecosystems due to their ubiquitous occurrence and documented adverse effects on non-target organisms. Despite the remarkable efforts to elucidate bioaccumulation and ecotoxicological potential under short-term conditions, limited and fragmentary information is available for chronic exposures. In this study bioavailability, molecular and cellular effects of diclofenac (DIC), ibuprofen (IBU) and ketoprofen (KET) were investigated in mussels Mytilus galloprovincialis exposed to the realistic environmental concentration of 2...

Over-the-counter (OTC) analgesics are routinely used worldwide for self-management of various painful conditions. Despite this, there has been little in-depth review of the safety of non-aspirin analgesics at OTC doses. This paper reviews the available literature on the gastrointestinal (GI) and hepatic safety of non-aspirin OTC analgesics, including nonsteroidal anti-inflammatory drugs (NSAIDs; ibuprofen, ketoprofen, diclofenac, and naproxen) and acetaminophen; safety in overdose is also reviewed. Each non-aspirin OTC analgesic has a distinct adverse event (AE) profile, with GI AE rates for OTC dosing in one study ranging from 37% for diclofenac to 7...

In the present work novel drug delivery systems consisting in highly porous Hyaluronan foams for the administration of a non-steroidal anti-inflammatory drug (NSAID), ketoprofen, have been obtained. A sugar-derived surfactant associated with ketoprofen was prepared and incorporated into the porous hyaluronan materials. The association between a lactose derived surfactant, Lhyd12, and ketoprofen was obtained by acid-base reaction and its physicochemical properties were studied. Tensiometric and dynamic light scattering (DLS) determinations showed the formation of catanionic surfactant aggregates, Lhyd12/ketoprofen, in aqueous solution...

It was the aim of this study to elucidate the impact of the injection mold temperature upon the polymer crystallinity, its microstructure and the resulting drug release from immediate and sustained release tablets containing semi-crystalline polymers. The immediate release formulation contained 20% (w/w) ketoprofen (KETO) in poly (ethylene oxide) (PEO) and the sustained release formulation contained 20 - 40% (w/w) metoprolol tartrate (MPT) in polycaprolactone (PCL). Physical mixtures of drug-polymer were characterized via isothermal crystallization experiments using DSC and rheological measurements to elucidate the impact of the drug solid-state upon the crystallization kinetics...

Herein, we propose the fabrication of a new carrier with core/shell structure-inner core of cellulose acetate (CA) coated by a micrometric layer of chitosan (CS)-fabricated through an integrated process, which combines Electro Dynamic Atomization (EDA) and layer-by-layer (LbL) technique. We demonstrate that CA based microspheres possess a unique capability to relevantly retain the drugs-that is, Ketoprofen Lysinate (KL)-along the gastric tract, while providing a massive release along the intestine. CS shell slightly influences the morphology and water retention under different pH conditions, improving drug encapsulation without compromising drug release kinetics...

The purpose of the present study was to determine whether caffeine modifies the pharmacokinetics and pharmacodynamics of (S)-ketoprofen following oral administration in a gout-type pain model. 3.2 mg/kg of (S)-ketoprofen alone and combined with 17.8 mg/kg of caffeine were administered to Wistar rats and plasma levels were determined between 0.5 and 24.0 h. Additionally, antinociception was evaluated based on the protocol of the PIFIR (pain-induced functional impairment in the rat) model before blood sampling between 0...

Background: Venipuncture pain is an uncomfortable suffering to the patient. It creates anxiety, fear and dissatisfaction. The ketoprofen transdermal patch is a proven treatment for musculoskeletal and arthritic pain. We planned this study to evaluate the efficacy of the ketoprofen patch to reduce venipuncture pain. Methods: Two hundred adult patients, aged 18-60 years, of either sex, ASA grade I or II, were enrolled. Presuming that therapy would decrease venipuncture pain by 30%, a power calculation with α = 0...

We investigated the effects of the addition of two coagulants-polyaluminium chloride (PACl) and chitosan-into the membrane bioreactor (MBR) process on membrane fouling and the removal of pharmaceuticals and personal care products (PPCPs). Their addition at optimized dosages improved the permeability of the membrane by reducing the concentration of soluble microbial products in mixed liquor, the content of inorganic elements, and irreversible fouling of the membrane surface. During long-term operation, the addition of PACl increased removal efficiencies of tetracycline, mefenamic acid, atenolol, furosemide, ketoprofen, and diclofenac by 17-23%...

CONTEXT: The role of prophylaxis for postoperative nausea and vomiting (PONV) in cardiac surgery is under debate. AIMS: To study the risk factors for PONV after cardiac surgery and the role of betamethasone with or without droperidol for its prevention. SETTING AND DESIGN: Randomized open-label controlled study comparing standard care with PONV prophylaxis from February to November 2016. METHODS: Five hundred and two patients with planned nonemergent cardiac surgery were included...

This work aims to evaluate the possible use of a poly(sodium methacrylate, methyl methacrylate) (NaPMM2) plasticized by PEG400 in design orodispersible films (ODF). Placebo ODF prepared by solvent casting were intended to study the impact of the polymer/plasticizer ratio and residual moisture on disintegration time, stickiness and mechanical properties. The drug loading capacity was assessed using ketoprofen and paracetamol. Placebo ODF containing PEG400 in the 10-30% w/w range and 10-15% of residual moisture content were easy-to-handle, packed without failures and completely dissolved within 30 s...

BACKGROUND: Inflammation has been implicated in many disorders, including cancer and available therapies elicit adverse effects. Plants of the family Rubiaceae have shown potency against inflammation. The anti-inflammatory and anti-oxidant potential of Feretia apodanthera was investigated in this study to evaluate its effectiveness. METHODS: The phytochemical, antioxidant and anti-inflammatory potential of root bark (n-Hexane, diethyl ether, ethanol and aqueous) extracts of Feretia apodanthera was investigated in this study...